Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T00156 | Target Info | |||
| Target Name | Short transient receptor potential channel 5 (TRPC5) | ||||
| Synonyms | hTRP5; hTRP-5; TrpC5; Transient receptor protein 5; TRP-5 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | TRPC5 | ||||
| Biochemical Class | Transient receptor potential catioin channel | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Riluzole | Ligand Info | |||||
| Structure Description | Human TRPC5 channel in complex with riluzole | PDB:7WDB | ||||
| Method | Electron microscopy | Resolution | 2.40 Å | Mutation | No | [1] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYQFSEFTPD 142 ITPIMLAAHT152 NNYEIIKLLV162 QKRVTIPRPH172 QIRCNCVECV182 SSSEVDSLRH 192 SRSRLNIYKA202 LASPSLIALS212 SEDPILTAFR222 LGWELKELSK232 VENEFKAEYE 242 ELSQQCKLFA252 KDLLDQARSS262 RELEIILNHR272 DDLAKLKVAI294 KYHQKEFVAQ 304 PNCQQLLATL314 WYDGFPGWRR324 KHWVVKLLTC334 MTIGFLFPML344 SIAYLISPRS 354 NLGLFIKKPF364 IKFICHTASY374 LTFLFMLLLA384 SQHVQGPPPT401 VVEWMILPWV 411 LGFIWGEIKE421 MWDGGFTEYI431 HDWWNLMDFA441 MNSLYLATIS451 LKIVAYVKYN 461 GSRPREEWEM471 WHPTLIAEAL481 FAISNILSSL491 RLISLFTANS501 HLGPLQISLG 511 RMLLDILKFL521 FIYCLVLLAF531 ANGLNQLYFY541 YETRAIDEPN551 NCKGIRCEKQ 561 NNAFSTLFET571 LQSLFWSVFG581 LLNLYVTNVK591 ARHEFTEFVG601 ATMFGTYNVI 611 SLVVLLNMLI621 AMMNNSYQLI631 ADHADIEWKF641 ARTKLWMSYF651 DEGGTLPPPF 661 NIISLIQNQH712 YQEVIRNLVK722 RYVAAMIRNS732 KTTEENFKEL746 KQDISSFRYE 756 VLDLL
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| Ligand Name: Clemizole | Ligand Info | |||||
| Structure Description | Structure of human TRPC5 in complex with clemizole | PDB:7D4P | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [2] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYTQFSEFTP 141 DITPIMLAAH151 TNNYEIIKLL161 VQKRVTIPRP171 HQIRCNCVEC181 VSSSEVDSLR 191 HSRSRLNIYK201 ALASPSLIAL211 SSEDPILTAF221 RLGWELKELS231 KVENEFKAEY 241 EELSQQCKLF251 AKDLLDQARS261 SRELEIILNH271 RDDLAKLKVA293 IKYHQKEFVA 303 QPNCQQLLAT313 LWYDGFPGWR323 RKHWVVKLLT333 CMTIGFLFPM343 LSIAYLISPR 353 SNLGLFIKKP363 FIKFICHTAS373 YLTFLFMLLL383 ASQDLHVQGP398 PPTVVEWMIL 408 PWVLGFIWGE418 IKEMWDGGFT428 EYIHDWWNLM438 DFAMNSLYLA448 TISLKIVAYV 458 KYNGSRPREE468 WEMWHPTLIA478 EALFAISNIL488 SSLRLISLFT498 ANSHLGPLQI 508 SLGRMLLDIL518 KFLFIYCLVL528 LAFANGLNQL538 YFYYETRAID548 EPNNCKGIRC 558 EKQNNAFSTL568 FETLQSLFWS578 VFGLLNLYVT588 NVKARHEFTE598 FVGATMFGTY 608 NVISLVVLLN618 MLIAMMNNSY628 QLIADHADIE638 WKFARTKLWM648 SYFDEGGTLP 658 PPFNIISLIQ709 NQHYQEVIRN719 LVKRYVAAMI729 RNSKTTEENF743 KELKQDISSF 753 RYEVLDLLG
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| Ligand Name: phosphatidylethanolamine | Ligand Info | |||||
| Structure Description | Human TRPC5 channel in complex with riluzole | PDB:7WDB | ||||
| Method | Electron microscopy | Resolution | 2.40 Å | Mutation | No | [1] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYQFSEFTPD 142 ITPIMLAAHT152 NNYEIIKLLV162 QKRVTIPRPH172 QIRCNCVECV182 SSSEVDSLRH 192 SRSRLNIYKA202 LASPSLIALS212 SEDPILTAFR222 LGWELKELSK232 VENEFKAEYE 242 ELSQQCKLFA252 KDLLDQARSS262 RELEIILNHR272 DDLAKLKVAI294 KYHQKEFVAQ 304 PNCQQLLATL314 WYDGFPGWRR324 KHWVVKLLTC334 MTIGFLFPML344 SIAYLISPRS 354 NLGLFIKKPF364 IKFICHTASY374 LTFLFMLLLA384 SQHVQGPPPT401 VVEWMILPWV 411 LGFIWGEIKE421 MWDGGFTEYI431 HDWWNLMDFA441 MNSLYLATIS451 LKIVAYVKYN 461 GSRPREEWEM471 WHPTLIAEAL481 FAISNILSSL491 RLISLFTANS501 HLGPLQISLG 511 RMLLDILKFL521 FIYCLVLLAF531 ANGLNQLYFY541 YETRAIDEPN551 NCKGIRCEKQ 561 NNAFSTLFET571 LQSLFWSVFG581 LLNLYVTNVK591 ARHEFTEFVG601 ATMFGTYNVI 611 SLVVLLNMLI621 AMMNNSYQLI631 ADHADIEWKF641 ARTKLWMSYF651 DEGGTLPPPF 661 NIISLIQNQH712 YQEVIRNLVK722 RYVAAMIRNS732 KTTEENFKEL746 KQDISSFRYE 756 VLDLL
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PTY or .PTY2 or .PTY3 or :3PTY;style chemicals stick;color identity;select .A:434 or .A:435 or .A:437 or .A:438 or .A:441 or .A:484 or .A:487 or .A:488 or .A:491 or .A:494 or .A:507 or .A:510 or .A:511 or .A:514; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Human TRPC5 channel in complex with riluzole | PDB:7WDB | ||||
| Method | Electron microscopy | Resolution | 2.40 Å | Mutation | No | [1] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYQFSEFTPD 142 ITPIMLAAHT152 NNYEIIKLLV162 QKRVTIPRPH172 QIRCNCVECV182 SSSEVDSLRH 192 SRSRLNIYKA202 LASPSLIALS212 SEDPILTAFR222 LGWELKELSK232 VENEFKAEYE 242 ELSQQCKLFA252 KDLLDQARSS262 RELEIILNHR272 DDLAKLKVAI294 KYHQKEFVAQ 304 PNCQQLLATL314 WYDGFPGWRR324 KHWVVKLLTC334 MTIGFLFPML344 SIAYLISPRS 354 NLGLFIKKPF364 IKFICHTASY374 LTFLFMLLLA384 SQHVQGPPPT401 VVEWMILPWV 411 LGFIWGEIKE421 MWDGGFTEYI431 HDWWNLMDFA441 MNSLYLATIS451 LKIVAYVKYN 461 GSRPREEWEM471 WHPTLIAEAL481 FAISNILSSL491 RLISLFTANS501 HLGPLQISLG 511 RMLLDILKFL521 FIYCLVLLAF531 ANGLNQLYFY541 YETRAIDEPN551 NCKGIRCEKQ 561 NNAFSTLFET571 LQSLFWSVFG581 LLNLYVTNVK591 ARHEFTEFVG601 ATMFGTYNVI 611 SLVVLLNMLI621 AMMNNSYQLI631 ADHADIEWKF641 ARTKLWMSYF651 DEGGTLPPPF 661 NIISLIQNQH712 YQEVIRNLVK722 RYVAAMIRNS732 KTTEENFKEL746 KQDISSFRYE 756 VLDLL
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .Y01 or .Y012 or .Y013 or :3Y01;style chemicals stick;color identity;select .A:315 or .A:316 or .A:322 or .A:364 or .A:367 or .A:368 or .A:371 or .A:375 or .A:493 or .A:496 or .A:497 or .A:499 or .A:500 or .A:501 or .A:503; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: [2-hydroxy-3-[(E)-octadec-10-enoyl]oxypropyl] (E)-octadec-10-enoate | Ligand Info | |||||
| Structure Description | Human TRPC5 channel in complex with riluzole | PDB:7WDB | ||||
| Method | Electron microscopy | Resolution | 2.40 Å | Mutation | No | [1] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYQFSEFTPD 142 ITPIMLAAHT152 NNYEIIKLLV162 QKRVTIPRPH172 QIRCNCVECV182 SSSEVDSLRH 192 SRSRLNIYKA202 LASPSLIALS212 SEDPILTAFR222 LGWELKELSK232 VENEFKAEYE 242 ELSQQCKLFA252 KDLLDQARSS262 RELEIILNHR272 DDLAKLKVAI294 KYHQKEFVAQ 304 PNCQQLLATL314 WYDGFPGWRR324 KHWVVKLLTC334 MTIGFLFPML344 SIAYLISPRS 354 NLGLFIKKPF364 IKFICHTASY374 LTFLFMLLLA384 SQHVQGPPPT401 VVEWMILPWV 411 LGFIWGEIKE421 MWDGGFTEYI431 HDWWNLMDFA441 MNSLYLATIS451 LKIVAYVKYN 461 GSRPREEWEM471 WHPTLIAEAL481 FAISNILSSL491 RLISLFTANS501 HLGPLQISLG 511 RMLLDILKFL521 FIYCLVLLAF531 ANGLNQLYFY541 YETRAIDEPN551 NCKGIRCEKQ 561 NNAFSTLFET571 LQSLFWSVFG581 LLNLYVTNVK591 ARHEFTEFVG601 ATMFGTYNVI 611 SLVVLLNMLI621 AMMNNSYQLI631 ADHADIEWKF641 ARTKLWMSYF651 DEGGTLPPPF 661 NIISLIQNQH712 YQEVIRNLVK722 RYVAAMIRNS732 KTTEENFKEL746 KQDISSFRYE 756 VLDLL
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .7OC or .7OC2 or .7OC3 or :37OC;style chemicals stick;color identity;select .A:514 or .A:520 or .A:521 or .A:524 or .A:525 or .A:528 or .A:557 or .A:569 or .A:572 or .A:573 or .A:576 or .A:577 or .A:579 or .A:617; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 1-Oleoyl-2-palmitoyl-sn-glycerol | Ligand Info | |||||
| Structure Description | Structure of human TRPC5 in complex with clemizole | PDB:7D4P | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [2] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYTQFSEFTP 141 DITPIMLAAH151 TNNYEIIKLL161 VQKRVTIPRP171 HQIRCNCVEC181 VSSSEVDSLR 191 HSRSRLNIYK201 ALASPSLIAL211 SSEDPILTAF221 RLGWELKELS231 KVENEFKAEY 241 EELSQQCKLF251 AKDLLDQARS261 SRELEIILNH271 RDDLAKLKVA293 IKYHQKEFVA 303 QPNCQQLLAT313 LWYDGFPGWR323 RKHWVVKLLT333 CMTIGFLFPM343 LSIAYLISPR 353 SNLGLFIKKP363 FIKFICHTAS373 YLTFLFMLLL383 ASQDLHVQGP398 PPTVVEWMIL 408 PWVLGFIWGE418 IKEMWDGGFT428 EYIHDWWNLM438 DFAMNSLYLA448 TISLKIVAYV 458 KYNGSRPREE468 WEMWHPTLIA478 EALFAISNIL488 SSLRLISLFT498 ANSHLGPLQI 508 SLGRMLLDIL518 KFLFIYCLVL528 LAFANGLNQL538 YFYYETRAID548 EPNNCKGIRC 558 EKQNNAFSTL568 FETLQSLFWS578 VFGLLNLYVT588 NVKARHEFTE598 FVGATMFGTY 608 NVISLVVLLN618 MLIAMMNNSY628 QLIADHADIE638 WKFARTKLWM648 SYFDEGGTLP 658 PPFNIISLIQ709 NQHYQEVIRN719 LVKRYVAAMI729 RNSKTTEENF743 KELKQDISSF 753 RYEVLDLLG
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .YZY or .YZY2 or .YZY3 or :3YZY;style chemicals stick;color identity;select .A:514 or .A:520 or .A:521 or .A:524 or .A:525 or .A:528 or .A:557 or .A:569 or .A:572 or .A:573 or .A:576 or .A:577 or .A:579 or .A:612 or .A:617; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 8-(3-Chloranylphenoxy)-7-[(4-chlorophenyl)methyl]-3-methyl-1-(3-oxidanylpropyl)purine-2,6-dione | Ligand Info | |||||
| Structure Description | Structure of human TRPC5 in complex with HC-070 | PDB:7D4Q | ||||
| Method | Electron microscopy | Resolution | 2.74 Å | Mutation | No | [2] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYTQFSEFTP 141 DITPIMLAAH151 TNNYEIIKLL161 VQKRVTIPRP171 HQIRCNCVEC181 VSSSEVDSLR 191 HSRSRLNIYK201 ALASPSLIAL211 SSEDPILTAF221 RLGWELKELS231 KVENEFKAEY 241 EELSQQCKLF251 AKDLLDQARS261 SRELEIILNH271 RDDLAKLKVA293 IKYHQKEFVA 303 QPNCQQLLAT313 LWYDGFPGWR323 RKHWVVKLLT333 CMTIGFLFPM343 LSIAYLISPR 353 SNLGLFIKKP363 FIKFICHTAS373 YLTFLFMLLL383 ASQDLHVQGP398 PPTVVEWMIL 408 PWVLGFIWGE418 IKEMWDGGFT428 EYIHDWWNLM438 DFAMNSLYLA448 TISLKIVAYV 458 KYNGSRPREE468 WEMWHPTLIA478 EALFAISNIL488 SSLRLISLFT498 ANSHLGPLQI 508 SLGRMLLDIL518 KFLFIYCLVL528 LAFANGLNQL538 YFYYETRAID548 EPNNCKGIRC 558 EKQNNAFSTL568 FETLQSLFWS578 VFGLLNLYVT588 NVKARHEFTE598 FVGATMFGTY 608 NVISLVVLLN618 MLIAMMNNSY628 QLIADHADIE638 WKFARTKLWM648 SYFDEGGTLP 658 PPFNIISLIQ709 NQHYQEVIRN719 LVKRYVAAMI729 RNSKTTEENF743 KELKQDISSF 753 RYEVLDLL
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .GWR or .GWR2 or .GWR3 or :3GWR;style chemicals stick;color identity;select .A:521 or .A:524 or .A:525 or .A:528 or .A:557 or .A:569 or .A:572 or .A:573 or .A:576 or .A:577; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural identification of riluzole-binding site on human TRPC5. Cell Discov. 2022 Jul 12;8(1):67. | ||||
| REF 2 | Structural basis for human TRPC5 channel inhibition by two distinct inhibitors. Elife. 2021 Mar 8;10:e63429. | ||||
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